Table 2.

SAR of N,N-disubstituted amide analogues (S,R)-1b, 2a-f

Comp.	R	IC50 Plm IV, μΜ	IC50 Cat D, μΜ	Sa
(S,R)-1b	n-Pr	0.024b	0.042b	1.8
(S,R)-2a	Et	0.014	0.25	17.9
(S,R)-2b	Me	0.087	0.5	5.7
(S,R)-2c	HOCH2CH2	0.068	0.27	4.0
(S,R)-2d	MeOCH2CH2	0.037	0.10	2.7
(S,R)-2e	CF3CH2CH2	0.21	0.12	0.57
(S,R)-2f	(CH3)2CHCH2	0.5	1.3	2.6

^aSelectivity factor of Plm IV/Cat D inhibition.

^bData from literature [11].